This report is the first part of an updated review of a previous survey published in this journal (2002, 2, 419-439). Since the discovery of the Human Genome Project dramatically increased our knowledge in regard of the mutated cancer cell, it is worthy to follow up those findings, that have brought progress in the therapy of malignant diseases. The molecular targeted drug therapy with transtuzumab or imatinib produced great initial success and several other candidate agents are now available for cancer treatment. This review summarises the antitumour effect of compounds under clinical testing. In the extracellular space, antiangiogenic molecules inhibit the metastasis production. Anti-MMP-s currently investigated are listed, followed by drugs designed to block endothelial proliferation. Membrane receptor blockers, signal transduction inhibitors, DNA replication inactivators, revertants and apoptosis inducers act in the intracellular space. Amongst these, proteasome inhibitors are of particular interest. This part of the review deals only with antiangiogenic products and the membrane receptor inhibitors. All other agents will be reviewed in the next part of this publication.